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Aminopeptidase N

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1560

Nomenclature: Aminopeptidase N

Family: M1: Aminopeptidase N

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 967 15q26.1 ANPEP alanyl aminopeptidase, membrane
Mouse 1 966 7 D2 Anpep alanyl aminopeptidase, membrane
Rat 1 965 1q31 Anpep alanyl aminopeptidase, membrane
Previous and Unofficial Names Click here for help
Alanyl aminopeptidase | gp150 | microsomal aminopeptidase | myeloid plasma membrane glycoprotein CD13 | LAP1 | aminopeptidase M | aminopeptidase N | AP-M | APN | cluster of differentiation antigen 13 (CD13) | kidney aminopeptidase M | kidney Zn peptidase | KZP | leucine arylaminopeptidase 1 | membrane alanine aminopeptidase | alanyl (membrane) aminopeptidase | alanyl aminopeptidase, membrane | alanyl aminopeptidase
Database Links Click here for help
Specialist databases
MEROPS M01.001 (Hs)
Other databases
Alphafold P15144 (Hs), P97449 (Mm), P15684 (Rn)
BRENDA 3.4.11.2
ChEMBL Target CHEMBL1907 (Hs), CHEMBL2189140 (Mm), CHEMBL3259 (Rn)
Ensembl Gene ENSG00000166825 (Hs), ENSMUSG00000039062 (Mm), ENSRNOG00000014610 (Rn)
Entrez Gene 290 (Hs), 81641 (Rn)
Human Protein Atlas ENSG00000166825 (Hs)
KEGG Enzyme 3.4.11.2
KEGG Gene hsa:290 (Hs), rno:81641 (Rn)
OMIM 151530 (Hs)
Pharos P15144 (Hs)
RefSeq Nucleotide NM_001150 (Hs), NM_008486 (Mm), NM_031012 (Rn)
RefSeq Protein NP_001141 (Hs), NP_032512 (Mm), NP_112274 (Rn)
UniProtKB P15144 (Hs), P97449 (Mm), P15684 (Rn)
Wikipedia ANPEP (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.11.2

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound I3 [PMID: 23428964] Small molecule or natural product Mm Inhibition 9.7 pKi 7
⤷ pKi 9.7 (Ki 2x10-10 M) [7]
compound I3 [PMID: 23428964] Small molecule or natural product Primary target of this compound Hs Inhibition 9.5 pKi 7
⤷ pKi 9.5 (Ki 3.5x10-10 M) [7]
compound 1a [PMID: 25692029] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pKi 2-3
⤷ pKi 8.5 (Ki 2.9x10-9 M) [2-3]
BTB07018 Small molecule or natural product Hs Inhibition 6.0 pKi 5
⤷ pKi 6.0 (Ki 1.01x10-6 M) [5]
Description: Inhibition of APN in vitro.
BTB07018 Small molecule or natural product Pig Inhibition 5.7 pKi 5
⤷ pKi 5.7 (Ki 1.95x10-6 M) [5]
JFD00064 Small molecule or natural product Hs Inhibition 5.7 pKi 5
⤷ pKi 5.7 (Ki 2.01x10-6 M) [5]
Description: Inhibition of APN in vitro.
JFD00064 Small molecule or natural product Pig Inhibition 5.5 pKi 5
⤷ pKi 5.5 (Ki 2.9x10-6 M) [5]
opiorphin Peptide Hs Inhibition 5.1 pIC50 6
⤷ pIC50 5.1 (IC50 8x10-6 M) [6]
View species-specific inhibitor tables
Immunopharmacology Comments
Pharmacological inhibitors of APN are being investigated to counter the dysregulated APN expression that has been associated with inflammatory diseases [1,4].
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cellular signalling
Immuno Process:  Barrier integrity
General Comments
APN (ANPEP) is a neutral metallo-aminopeptidase that catalyses the removal of neutral and basic amino acids from the N-terminus of protein or peptide substrates. Since dysregulated APN expression has been associated with inflammatory diseases and some types of cancer, pharmacological inhibition of APN may offer effective therapy for these indications.

References

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1. Bauvois B, Dauzonne D. (2006) Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: chemistry, biological evaluations, and therapeutic prospects. Med Res Rev, 26 (1): 88-130. [PMID:16216010]

2. Bonnard E, Poras H, Nadal X, Maldonado R, Fournié-Zaluski MC, Roques BP. (2015) Long-lasting oral analgesic effects of N-protected aminophosphinic dual ENKephalinase inhibitors (DENKIs) in peripherally controlled pain. Pharmacol Res Perspect, 3 (2): e00116. [PMID:25692029]

3. Chen H, Noble F, Roques BP, Fournié-Zaluski MC. (2001) Long lasting antinociceptive properties of enkephalin degrading enzyme (NEP and APN) inhibitor prodrugs. J Med Chem, 44 (21): 3523-30. [PMID:11585456]

4. Luan Y, Xu W. (2007) The structure and main functions of aminopeptidase N. Curr Med Chem, 14 (6): 639-47. [PMID:17346152]

5. Pascual I, Valiente PA, García G, Valdés-Tresanco ME, Arrebola Y, Díaz L, Bounaadja L, Uribe RM, Pacheco MC, Florent I et al.. (2017) Discovery of novel non-competitive inhibitors of mammalian neutral M1 aminopeptidase (APN). Biochimie, 142: 216-225. [PMID:28964831]

6. Pinto M, Rougeot C, Gracia L, Rosa M, García A, Arsequell G, Valencia G, Centeno NB. (2012) Proposed Bioactive Conformations of Opiorphin, an Endogenous Dual APN/NEP Inhibitor. ACS Med Chem Lett, 3 (1): 20-4. [PMID:24900367]

7. Schmitt C, Voegelin M, Marin A, Schmitt M, Schegg F, Hénon P, Guenot D, Tarnus C. (2013) Selective aminopeptidase-N (CD13) inhibitors with relevance to cancer chemotherapy. Bioorg Med Chem, 21 (7): 2135-44. [PMID:23428964]

How to cite this page

M1: Aminopeptidase N: Aminopeptidase N. Last modified on 11/05/2021. Accessed on 23/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1560.